Peringatan Keamanan

> 7 g/kg ( Rat ) L2382

Common adverse reactions

The most commonly reported adverse reaction during treatment is diarrhea L2371. High doses of Vitamin E may cause diarrhea, abdominal pain, and other gastrointestinal conditions. In the case of an overdose, symptomatic treatment should be provided L2371. High doses of vitamin E have been reported to increase bleeding tendency in patients with Vitamin K deficiency, or patients taking oral anti-vitamins K treatment L2371. Therefore, careful monitoring of the prothrombin time and international normalized ratio (INR) are advised. A possible adjustment of the dose of oral anticoagulant during and after treatment with Vedrop may be necessary L2371.

Renal impairment

Data regarding patients with renal impairment are limited, this drug should be administered with caution and those with renal impairment or dehydration should be closely followed L2371.

Hepatic impairment

This drug should be administered with caution in patients with liver impairment and under close monitoring of the liver function tests in such patients L2371.

Hypersensitivity

Vedrop, the commercial form, contains sodium methyl parahydroxybenzoate (E219) and sodium ethyl parahydroxybenzoate (E215) which may cause allergic reactions, which are sometimes delayed L2371.

Pregnancy

There is no current data on taking tocofersolan during pregnancy. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/ fetal development, parturition or postnatal development. Caution should be taken when prescribing this medication to pregnant women L2371.

Breast-feeding

It is unknown whether tocofersolan is released into human breast milk. The excretion of tocofersolan in milk has not been studied in animals L2371.

Fertility

No data is available L2371.

Tocofersolan

DB11635

small molecule approved

Deskripsi

D-Alpha-tocopheryl polyethylene glycol 1000 succinate (Tocofersolan, Vedrop), has been developed in Europe as an orally bioavailable source of vitamin E in children suffering from cholestasis L2371. Cholestasis is the reduction or stoppage of bile flow, either to impaired secretion by hepatocytes (liver cells) or obstruction L2374, L2375.

Tocofersolan is a polyethylene glycol derivative of ?-tocopherol and synthetic water-soluble version of DB11251. Tocofersolan is an oral treatment of vitamin E deficiency due to digestive malabsorption in pediatric patients with congenital chronic cholestasis or hereditary chronic cholestasis. It was approved by the European Medicines Agency (EMA) in June 2009 under the market name Vedrop. Moreover, the agent is capable of demonstrating antioxidant effects that make it a popular component to include in cosmetics and pharmaceuticals as well.

In addition to the above, tocofersolan has been studied as a promising application as an absorption enhancer in drug delivery MSDS.

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 29.7 h [L2371]
Volume Distribusi Located principally on cell membranes, within mitochondria and microsomes, vitamin E is widely distributed throughout the body (red blood cells, brain, muscle, liver, platelets) and fat tissues are its primary reservoir [L2371].
Klirens (Clearance) -

Absorpsi

The bioavailability of vitamin E from tocofersolan is unique from than that of other medicinal products L2371. Due to its amphipathic property in which it forms its own micelles, tocofersolan is readily taken up into enterocytes, even in the absence of bile salts; fat-soluble d-alpha-tocopherol is then released after hydrolysis. This formulation enhances the absorption of d-alpha-tocopherol compared to the administration of free d-alpha-tocopherol. Additionally, tocophersolan may enhance the absorption of water-insoluble agents and other fat-soluble vitamins L2376. Tocofersolan is a pro-drug; the active metabolite is the d-alpha-tocopherol. At low concentrations, tocofersolan forms micelles which improve the absorption of non-polar lipids such as other fat-soluble vitamins. Its required micellar concentration is low (0.04 to 0.06 mmol/l) L2371. A pharmacokinetic study of 12 healthy subjects compared tocofersolan with a water-miscible reference vitamin E after one single oral loading dose of 1200 IU (international units). The relative bioavailability of tocofersolan was found to be (Frel of 1.01 ± 1.74) with AUC0-t of 0.383 ± 0.203?M.h/mg, Cmax of 0.013 ± 0.006, Tmax of 6.0 h (6.0 – 24.0) L2371. For more information about Vitamin E metabolism, please visit the drug entry DB11251.

Metabolisme

The hydrolysis of tocofersolan occurs in the gut lumen. Tocofersolan is absorbed by cells, and the alpha-tocopherol moiety appears in chylomicrons in the lymph system in a manner that is identical to vitamin E absorbed from dietary sources. Cellular uptake does not require receptors, binding proteins or metabolic processes and does not occur by pinocytosis. Absorption of deuterated tocofersolan demonstrated a normal pattern in lipoproteins: alpha-tocopherol peaked first in chylomicrons, then peaked in very low- density lipoproteins (VLDL) and finally in low-density lipoproteins (LDL) and high-density lipoproteins (HDL)L2371.

Rute Eliminasi

Vitamin E is primarily eliminated in the bile (75%) and feces, either as free tocopherol or in oxidized forms. Urine is a minor elimination route of vitamin E (as glucuronic-conjugate) L2371.

Interaksi Obat

107 Data
Orlistat Orlistat can cause a decrease in the absorption of Tocofersolan resulting in a reduced serum concentration and potentially a decrease in efficacy.
Pitolisant The serum concentration of Tocofersolan can be decreased when it is combined with Pitolisant.
Metreleptin The metabolism of Tocofersolan can be increased when combined with Metreleptin.
Cenobamate The serum concentration of Tocofersolan can be decreased when it is combined with Cenobamate.
Ritonavir The serum concentration of Tocofersolan can be increased when it is combined with Ritonavir.
Haloperidol The serum concentration of Haloperidol can be increased when it is combined with Tocofersolan.
Tucatinib The metabolism of Tucatinib can be decreased when combined with Tocofersolan.
Abametapir The serum concentration of Tocofersolan can be increased when it is combined with Abametapir.
Satralizumab The serum concentration of Tocofersolan can be decreased when it is combined with Satralizumab.
Sotorasib The serum concentration of Tocofersolan can be decreased when it is combined with Sotorasib.
Cyclosporine The metabolism of Tocofersolan can be decreased when combined with Cyclosporine.
Fluvoxamine The metabolism of Tocofersolan can be decreased when combined with Fluvoxamine.
Fluconazole The metabolism of Tocofersolan can be decreased when combined with Fluconazole.
Erythromycin The serum concentration of Tocofersolan can be increased when it is combined with Erythromycin.
Ziprasidone The metabolism of Tocofersolan can be decreased when combined with Ziprasidone.
Isradipine The metabolism of Tocofersolan can be decreased when combined with Isradipine.
Diltiazem The metabolism of Tocofersolan can be decreased when combined with Diltiazem.
Clozapine The metabolism of Tocofersolan can be decreased when combined with Clozapine.
Ciprofloxacin The metabolism of Tocofersolan can be decreased when combined with Ciprofloxacin.
Nicardipine The metabolism of Tocofersolan can be decreased when combined with Nicardipine.
Verapamil The metabolism of Tocofersolan can be decreased when combined with Verapamil.
Aprepitant The metabolism of Tocofersolan can be decreased when combined with Aprepitant.
Isoniazid The metabolism of Tocofersolan can be decreased when combined with Isoniazid.
Primaquine The metabolism of Tocofersolan can be decreased when combined with Primaquine.
Miconazole The metabolism of Tocofersolan can be decreased when combined with Miconazole.
Fusidic acid The metabolism of Tocofersolan can be decreased when combined with Fusidic acid.
Zimelidine The metabolism of Tocofersolan can be decreased when combined with Zimelidine.
Dronedarone The metabolism of Tocofersolan can be decreased when combined with Dronedarone.
Milnacipran The metabolism of Tocofersolan can be decreased when combined with Milnacipran.
Simeprevir The metabolism of Tocofersolan can be decreased when combined with Simeprevir.
Isavuconazonium The metabolism of Tocofersolan can be decreased when combined with Isavuconazonium.
Desvenlafaxine The metabolism of Tocofersolan can be decreased when combined with Desvenlafaxine.
Nilvadipine The metabolism of Tocofersolan can be decreased when combined with Nilvadipine.
Seproxetine The metabolism of Tocofersolan can be decreased when combined with Seproxetine.
Linagliptin The metabolism of Tocofersolan can be decreased when combined with Linagliptin.
Indalpine The metabolism of Tocofersolan can be decreased when combined with Indalpine.
Netupitant The metabolism of Tocofersolan can be decreased when combined with Netupitant.
Barnidipine The metabolism of Tocofersolan can be decreased when combined with Barnidipine.
Benidipine The metabolism of Tocofersolan can be decreased when combined with Benidipine.
Venetoclax The metabolism of Tocofersolan can be decreased when combined with Venetoclax.
Isavuconazole The metabolism of Tocofersolan can be decreased when combined with Isavuconazole.
Fosnetupitant The metabolism of Tocofersolan can be decreased when combined with Fosnetupitant.
Berotralstat The metabolism of Tocofersolan can be decreased when combined with Berotralstat.
Midostaurin The metabolism of Tocofersolan can be decreased when combined with Midostaurin.
Voriconazole The metabolism of Tocofersolan can be decreased when combined with Voriconazole.
Danazol The metabolism of Tocofersolan can be decreased when combined with Danazol.
Nelfinavir The metabolism of Tocofersolan can be decreased when combined with Nelfinavir.
Indinavir The metabolism of Tocofersolan can be decreased when combined with Indinavir.
Terfenadine The metabolism of Tocofersolan can be decreased when combined with Terfenadine.
Efavirenz The metabolism of Tocofersolan can be decreased when combined with Efavirenz.
Ergotamine The metabolism of Tocofersolan can be decreased when combined with Ergotamine.
Amprenavir The metabolism of Tocofersolan can be decreased when combined with Amprenavir.
Delavirdine The metabolism of Tocofersolan can be decreased when combined with Delavirdine.
Methimazole The metabolism of Tocofersolan can be decreased when combined with Methimazole.
Conivaptan The metabolism of Tocofersolan can be decreased when combined with Conivaptan.
Tipranavir The metabolism of Tocofersolan can be decreased when combined with Tipranavir.
Telithromycin The metabolism of Tocofersolan can be decreased when combined with Telithromycin.
Ketoconazole The metabolism of Tocofersolan can be decreased when combined with Ketoconazole.
Atazanavir The metabolism of Tocofersolan can be decreased when combined with Atazanavir.
Amiodarone The metabolism of Tocofersolan can be decreased when combined with Amiodarone.
Nefazodone The metabolism of Tocofersolan can be decreased when combined with Nefazodone.
Itraconazole The metabolism of Tocofersolan can be decreased when combined with Itraconazole.
Clarithromycin The metabolism of Tocofersolan can be decreased when combined with Clarithromycin.
Saquinavir The metabolism of Tocofersolan can be decreased when combined with Saquinavir.
Posaconazole The metabolism of Tocofersolan can be decreased when combined with Posaconazole.
Darunavir The metabolism of Tocofersolan can be decreased when combined with Darunavir.
Lopinavir The metabolism of Tocofersolan can be decreased when combined with Lopinavir.
Ditiocarb The metabolism of Tocofersolan can be decreased when combined with Ditiocarb.
Nilotinib The metabolism of Tocofersolan can be decreased when combined with Nilotinib.
Telaprevir The metabolism of Tocofersolan can be decreased when combined with Telaprevir.
Lonafarnib The metabolism of Tocofersolan can be decreased when combined with Lonafarnib.
Boceprevir The metabolism of Tocofersolan can be decreased when combined with Boceprevir.
Elvitegravir The metabolism of Tocofersolan can be decreased when combined with Elvitegravir.
Stiripentol The metabolism of Tocofersolan can be decreased when combined with Stiripentol.
Ribociclib The metabolism of Tocofersolan can be decreased when combined with Ribociclib.
Danoprevir The metabolism of Tocofersolan can be decreased when combined with Danoprevir.
Troleandomycin The metabolism of Tocofersolan can be decreased when combined with Troleandomycin.
Phenytoin The metabolism of Tocofersolan can be increased when combined with Phenytoin.
Pentobarbital The metabolism of Tocofersolan can be increased when combined with Pentobarbital.
Carbamazepine The metabolism of Tocofersolan can be increased when combined with Carbamazepine.
Mitotane The metabolism of Tocofersolan can be increased when combined with Mitotane.
Primidone The metabolism of Tocofersolan can be increased when combined with Primidone.
Rifampin The metabolism of Tocofersolan can be increased when combined with Rifampicin.
Phenobarbital The metabolism of Tocofersolan can be increased when combined with Phenobarbital.
Dexamethasone The metabolism of Tocofersolan can be increased when combined with Dexamethasone.
Fosphenytoin The metabolism of Tocofersolan can be increased when combined with Fosphenytoin.
St. John's Wort The metabolism of Tocofersolan can be increased when combined with St. John's Wort.
Enzalutamide The serum concentration of Tocofersolan can be decreased when it is combined with Enzalutamide.
Lumacaftor The metabolism of Tocofersolan can be increased when combined with Lumacaftor.
Apalutamide The serum concentration of Tocofersolan can be decreased when it is combined with Apalutamide.
Rifapentine The metabolism of Tocofersolan can be increased when combined with Rifapentine.
Curcumin The metabolism of Tocofersolan can be decreased when combined with Curcumin.
Somatrogon The metabolism of Tocofersolan can be increased when combined with Somatrogon.
Levoketoconazole The metabolism of Tocofersolan can be decreased when combined with Levoketoconazole.
Mavacamten The serum concentration of Tocofersolan can be decreased when it is combined with Mavacamten.
Viloxazine The metabolism of Tocofersolan can be decreased when combined with Viloxazine.
Ivosidenib The metabolism of Tocofersolan can be increased when combined with Ivosidenib.
Dabrafenib The serum concentration of Tocofersolan can be decreased when it is combined with Dabrafenib.
Telotristat ethyl The serum concentration of Tocofersolan can be decreased when it is combined with Telotristat ethyl.
Avanafil The serum concentration of Avanafil can be increased when it is combined with Tocofersolan.

Target Protein

ATP-dependent translocase ABCB1 ABCB1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 27429423
    Thebaut A, Nemeth A, Le Mouhaer J, Scheenstra R, Baumann U, Koot B, Gottrand F, Houwen R, Monard L, de Micheaux SL, Habes D, Jacquemin E: Oral Tocofersolan Corrects or Prevents Vitamin E Deficiency in Children With Chronic Cholestasis. J Pediatr Gastroenterol Nutr. 2016 Dec;63(6):610-615. doi: 10.1097/MPG.0000000000001331.
  • PMID: 12549795
    Roongpraiwan R, Suthutvoravut U, Feungpean B, Phuapradit P: Effect of oral vitamin E supplementation in children with cholestasis. J Med Assoc Thai. 2002 Nov;85 Suppl 4:S1199-205.

Contoh Produk & Brand

Produk: 6 • International brands: 0
Produk
  • Aquasol E Tpgs Liquid 77iu/ml
    Liquid • 77 unit / mL • Oral • Canada • OTC • Approved
  • NESTABS ABC Prenatal Multi-vitamin/Mineral Supplement with DHA/EPA
    Capsule, gelatin coated; Kit; Tablet • - • Oral • US
  • Pre-Tabs DHA Prenatal Multi-vitamin/Mineral Supplement with DHA/EPA
    Kit • - • Oral • US
  • Vedrop
    Solution • 50 mg/mL • Oral • EU • Approved
  • Vedrop
    Solution • 50 mg/mL • Oral • EU • Approved
  • Vedrop
    Solution • 50 mg/mL • Oral • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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